3-Propenyl derivatives of cephalosporin, compositions and their use
申请人:Syntex (U.S.A.) Inc.
公开号:US04094978A1
公开(公告)日:1978-06-13
3-(3-hydroxyprop-1-(t)-enyl)-7.beta.-(.alpha.-substituted acetamido)-ceph-3-em-4-carboxylic acids; 3-(3-carbamoyloxyprop-1-(t)-enyl)-7.beta.-(.alpha.-substituted acetamido)-ceph-3-em-4-carboxylic acids; and 3-[3-(N-substituted carbamoyloxy)prop-1-(t)-enyl]-7.beta.-(.alpha.-substituted acetamido)-ceph-3-em-4-carboxylic acids and derivatives and salts thereof and process for preparing such compounds. The compounds are useful as antibacterials and are active against a wide variety of gram positive and gram negative bacteria.
Tri-substituted aryl and heteroaryl derivatives as modulators of PI3-kinase and autophagy pathways
申请人:Neuropore Therapies, Inc.
公开号:US11492348B2
公开(公告)日:2022-11-08
The present disclosure relates to tri-substituted aryl and heteroaryl derivatives, pharmaceutical compositions containing them, and methods of using them, including methods for modulating autophagy or preventing, reversing, slowing or inhibiting the PI3K-AKT-MTOR pathway, and methods of treating diseases that are associated with autophagy or the PI3K-AKT-MTOR pathway.
In order to synthesise fragments of the natural product diazonamide A, alpha-arylation of 2-arylacetates 3 and benzofuran-2-one with the aid of the tricarbonyl(fluoroarene)chromium complex rac-2 was investigated. After decomplexation of the products rac-4 and rac-6, it was possible to obtain 2,2-diaryl-acetates rac-5 and the 3-arylbenzofuran-2-one rac-7.